4,5-Bis(2-sulfanylacetamido)pentanoic acid | 105655-82-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 4,5-Bis(2-sulfanylacetamido)pentanoic acid
• 英文别名: 4,5-bis[(2-sulfanylacetyl)amino]pentanoic acid
• CAS: 105655-82-1
• 化学式: C₉H₁₆N₂O₄S₂
• 分子量: 280.4
• InChiKey: GCLPVLHUUUBUED-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  17
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  97.5
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• Anchimeric radiometal chelating compounds
  申请人：NEORX CORPORATION

  公开号：EP0329481A2

  公开（公告）日：1989-08-23

  Anchimeric chelating compounds which are capable of rapidly forming stable chelates with radionuclide metals at or below physiological temperatures are disclosed. The compounds possess a first site capable of complexing with a radionuclide metal which can be transferred to a second site (to form a chelate) by incubation, such as at 37°C or below. These anchimeric chelating compounds may be bifunctional and so are useful for radiolabelling target specific molecules such as monoclonal antibodies and fragments thereof, that may be specific for cancer cells.

  本发明公开了能够在生理温度或生理温度以下与放射性核素金属迅速形成稳定螯合物的嵌合螯合化合物。这些化合物具有一个能与放射性核素金属络合的第一位点，通过培养，如在 37°C 或更低温度下培养，该位点可转移到第二位点（形成螯合物）。这些锚嵌螯合化合物可能具有双功能，因此可用于对癌细胞具有特异性的目标特异性分子（如单克隆抗体及其片段）进行放射性标记。
• Compounds for use in diagnosing and treating melanoma, including metastatic melanoma and methods related to same
  申请人：STC.UNM

  公开号：US10265425B2

  公开（公告）日：2019-04-23

  The present invention is directed to novel non-invasive diagnostic tools/compounds comprising a cyclic peptide wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention will also be useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.

  本发明涉及新型非侵入性诊断工具/化合物，它包含一种环肽，其中的化合物与 MSH 受体结合，用于对癌症，尤其是黑色素瘤（包括体内转移性黑色素瘤）进行成像和治疗。本发明代表了目前依靠组织活检诊断这些癌症的技术的明显进步。新型成像探针能够检测癌黑色素瘤细胞及其在组织中的转移扩散。这标志着利用无创分子成像技术诊断和治疗黑色素瘤（包括转移性黑色素瘤）向前迈进了一大步。本发明的新型探针还可用于启动黑色素瘤的治疗，以及监测患者对化疗和用于治疗黑色素瘤/转移性黑色素瘤的其他干预或疗法的反应。根据本发明的化合物可用作一些病症和疾病状态的诊断工具以及治疗这些病症和疾病状态的治疗剂。
• Compounds with reduced ring size for use in diagnosing and treating melanoma, including metastatic melanoma and methods related to same
  申请人：STC.UNM

  公开号：US10464985B2

  公开（公告）日：2019-11-05

  The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue and decreased renal uptake in kidney, evidencing favorable pharmacokinetics of compounds of the present invention. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are also useful for initiating therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.

  本发明涉及新型非侵入性诊断工具/化合物，用于对癌症，特别是黑色素瘤，包括转移性黑色素瘤进行体内成像。本发明化合物在癌细胞和组织中的吸收增强，在肾脏中的吸收降低，证明本发明化合物的药代动力学良好。本发明的化合物是利用非侵入性分子成像技术诊断和治疗黑色素瘤（包括转移性黑色素瘤）的一大进步。本发明的新型探针还可用于启动黑色素瘤的治疗，以及监测患者对化疗治疗和用于治疗黑色素瘤/转移性黑色素瘤的其他干预或疗法的反应。根据本发明的化合物可用作一些病症和疾病状态的诊断工具以及治疗这些病症和疾病状态的治疗剂。
• Control of chronic neuropathic pain and allodynia
  申请人：STC.UNM

  公开号：US10548994B1

  公开（公告）日：2020-02-04

  In one embodiment, the invention provides a method of treating a subject suffering from chronic neuropathic pain and/or allodynia by administering a therapeutically-effective amount of at least one LFA1 antagonist to the subject. In a preferred embodiment, the invention provides a method of treating a subject suffering from chronic neuropathic pain and/or allodynia, the method comprising administering intrathecally to the subject a therapeutically-effective amount of microparticles comprising PLGA-encapsulated pDNA-IL-10, optionally in combination with a therapeutically-effective amount of intrathecally-administered CpG oligodeoxynucleotide (CpG ODN) and/or at least one LFA1 antagonist.

  在一个实施方案中，本发明提供了一种治疗患有慢性神经病理性疼痛和/或异感症的受试者的方法，该方法通过向受试者施用治疗有效量的至少一种LFA1拮抗剂。在一个优选的实施方案中，本发明提供了一种治疗患有慢性神经病理性疼痛和/或异感症的受试者的方法，该方法包括向受试者经鞘内给药治疗有效量的微颗粒，该微颗粒包含PLGA包封的pDNA-IL-10，可选地与治疗有效量的经鞘内给药的CpG寡脱氧核苷酸（CpG ODN）和/或至少一种LFA1拮抗剂结合使用。
• Compositions for use in diagnosing and treating melanoma, including metastatic melanoma and methods related to same
  申请人：UNM RAINFOREST INNOVATIONS

  公开号：US11160887B2

  公开（公告）日：2021-11-02

  The present invention is directed to novel non-invasive diagnostic tools/compounds comprising a cyclic peptide wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention will also be useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.

  本发明涉及新型非侵入性诊断工具/化合物，它包含一种环肽，其中的化合物与 MSH 受体结合，用于对癌症，尤其是黑色素瘤（包括体内转移性黑色素瘤）进行成像和治疗。本发明代表了目前依靠组织活检诊断这些癌症的技术的明显进步。新型成像探针能够检测癌黑色素瘤细胞及其在组织中的转移扩散。这标志着利用无创分子成像技术诊断和治疗黑色素瘤（包括转移性黑色素瘤）向前迈进了一大步。本发明的新型探针还可用于启动黑色素瘤的治疗，以及监测患者对化疗和用于治疗黑色素瘤/转移性黑色素瘤的其他干预或疗法的反应。根据本发明的化合物可用作一些病症和疾病状态的诊断工具以及治疗这些病症和疾病状态的治疗剂。